Ionisation effects on the permeation of pharmaceutical compounds through silicone membrane

L. J. Waters, A. K M M H Bhuiyan

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Silicone membrane is frequently used as an in vitro skin mimic whereby experiments incorporate a range of buffered media which may vary in pH. As a consequence of such variability in pH there is a corresponding variability in the degree of ionisation which in turn, could influence permeation through the mainly hydrophobic-rich membrane structure. This study reports the effect of pH on the permeation of five model compounds (benzoic acid, benzotriazole, ibuprofen, ketoprofen and lidocaine). For the five compounds analysed, each at three distinct percentages of ionisation, it was found that the greater extent of permeation was always for the more 'neutral', i.e. more greatly unionised, species rather than the anionic or cationic species. These findings fit with the theory that the hydrophobic membrane encourages permeation of 'lipid-like' structures, i.e. the more unionised form of compounds. However, results obtained with an Inverse Gas Chromatography Surface Energy Analyser (iGC SEA) indicate the membrane surface to be an electron dense environment. In the knowledge that unionised forms of compounds permeate (rather than the charged species) this negatively charged surface was not anticipated, i.e. the basic membrane surface did not appear to affect permeation.

Original languageEnglish
Pages (from-to)553-557
Number of pages5
JournalColloids and Surfaces B: Biointerfaces
Volume141
Early online date1 Feb 2016
DOIs
Publication statusPublished - 1 May 2016

Fingerprint

silicones
Silicones
Permeation
Drug products
Ionization
membranes
Membranes
ionization
Pharmaceutical Preparations
membrane structures
benzoic acid
Ketoprofen
gas chromatography
Membrane structures
Benzoic Acid
Benzoic acid
Ibuprofen
surface energy
lipids
Lidocaine

Cite this

@article{d5a62a5408db413ea849b7eff448bcd2,
title = "Ionisation effects on the permeation of pharmaceutical compounds through silicone membrane",
abstract = "Silicone membrane is frequently used as an in vitro skin mimic whereby experiments incorporate a range of buffered media which may vary in pH. As a consequence of such variability in pH there is a corresponding variability in the degree of ionisation which in turn, could influence permeation through the mainly hydrophobic-rich membrane structure. This study reports the effect of pH on the permeation of five model compounds (benzoic acid, benzotriazole, ibuprofen, ketoprofen and lidocaine). For the five compounds analysed, each at three distinct percentages of ionisation, it was found that the greater extent of permeation was always for the more 'neutral', i.e. more greatly unionised, species rather than the anionic or cationic species. These findings fit with the theory that the hydrophobic membrane encourages permeation of 'lipid-like' structures, i.e. the more unionised form of compounds. However, results obtained with an Inverse Gas Chromatography Surface Energy Analyser (iGC SEA) indicate the membrane surface to be an electron dense environment. In the knowledge that unionised forms of compounds permeate (rather than the charged species) this negatively charged surface was not anticipated, i.e. the basic membrane surface did not appear to affect permeation.",
keywords = "Ionisation, PDMS, Permeation, PK, Silicone, Transdermal",
author = "Waters, {L. J.} and Bhuiyan, {A. K M M H}",
year = "2016",
month = "5",
day = "1",
doi = "10.1016/j.colsurfb.2016.01.055",
language = "English",
volume = "141",
pages = "553--557",
journal = "Colloids and Surfaces B: Biointerfaces",
issn = "0927-7765",
publisher = "Elsevier",

}

Ionisation effects on the permeation of pharmaceutical compounds through silicone membrane. / Waters, L. J.; Bhuiyan, A. K M M H.

In: Colloids and Surfaces B: Biointerfaces, Vol. 141, 01.05.2016, p. 553-557.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Ionisation effects on the permeation of pharmaceutical compounds through silicone membrane

AU - Waters, L. J.

AU - Bhuiyan, A. K M M H

PY - 2016/5/1

Y1 - 2016/5/1

N2 - Silicone membrane is frequently used as an in vitro skin mimic whereby experiments incorporate a range of buffered media which may vary in pH. As a consequence of such variability in pH there is a corresponding variability in the degree of ionisation which in turn, could influence permeation through the mainly hydrophobic-rich membrane structure. This study reports the effect of pH on the permeation of five model compounds (benzoic acid, benzotriazole, ibuprofen, ketoprofen and lidocaine). For the five compounds analysed, each at three distinct percentages of ionisation, it was found that the greater extent of permeation was always for the more 'neutral', i.e. more greatly unionised, species rather than the anionic or cationic species. These findings fit with the theory that the hydrophobic membrane encourages permeation of 'lipid-like' structures, i.e. the more unionised form of compounds. However, results obtained with an Inverse Gas Chromatography Surface Energy Analyser (iGC SEA) indicate the membrane surface to be an electron dense environment. In the knowledge that unionised forms of compounds permeate (rather than the charged species) this negatively charged surface was not anticipated, i.e. the basic membrane surface did not appear to affect permeation.

AB - Silicone membrane is frequently used as an in vitro skin mimic whereby experiments incorporate a range of buffered media which may vary in pH. As a consequence of such variability in pH there is a corresponding variability in the degree of ionisation which in turn, could influence permeation through the mainly hydrophobic-rich membrane structure. This study reports the effect of pH on the permeation of five model compounds (benzoic acid, benzotriazole, ibuprofen, ketoprofen and lidocaine). For the five compounds analysed, each at three distinct percentages of ionisation, it was found that the greater extent of permeation was always for the more 'neutral', i.e. more greatly unionised, species rather than the anionic or cationic species. These findings fit with the theory that the hydrophobic membrane encourages permeation of 'lipid-like' structures, i.e. the more unionised form of compounds. However, results obtained with an Inverse Gas Chromatography Surface Energy Analyser (iGC SEA) indicate the membrane surface to be an electron dense environment. In the knowledge that unionised forms of compounds permeate (rather than the charged species) this negatively charged surface was not anticipated, i.e. the basic membrane surface did not appear to affect permeation.

KW - Ionisation

KW - PDMS

KW - Permeation

KW - PK

KW - Silicone

KW - Transdermal

UR - http://www.scopus.com/inward/record.url?scp=84958259665&partnerID=8YFLogxK

U2 - 10.1016/j.colsurfb.2016.01.055

DO - 10.1016/j.colsurfb.2016.01.055

M3 - Article

VL - 141

SP - 553

EP - 557

JO - Colloids and Surfaces B: Biointerfaces

JF - Colloids and Surfaces B: Biointerfaces

SN - 0927-7765

ER -